Epizyme Earns $4 Million in Milestone Payments in GlaxoSmithKline Alliance to Discover and Develop Novel HMT Therapeutics

Alliance Focuses on Novel, Small Molecule Therapeutics Targeting Epigenetic Enzymes for the Treatment of Cancer and Other Diseases

CAMBRIDGE, Mass., Oct. 3, 2012 /PRNewswire-USNewswire/ -- Epizyme, Inc., a company leading the discovery and development of personalized therapeutics for patients with genetically defined cancers, announced today $4 million in milestone payments from collaborator GlaxoSmithKline (GSK) based on the achievement of pre-clinical milestones. In 2011, Epizyme and GSK formed a worldwide strategic alliance to discover, develop, and market novel small molecule therapeutics targeting histone methyltransferases (HMTs), an important class of epigenetic enzymes, for the treatment of cancer and other diseases.

These milestone payments follow $4 million in milestone payments from GSK to Epizyme in October 2011, bringing the total milestone payments to Epizyme to $8 million to date.

"This achievement reflects the rapid continued progress of our alliance with GSK and the power of Epizyme's platform to create small molecule histone methyltransferase inhibitors (HMTi) as personalized therapeutics for patients with genetically defined diseases," said Robert Copeland, Ph.D., Executive Vice President and Chief Scientific Officer, Epizyme. "We are excited to have GSK as a collaborator as we work together to bring new, personalized therapeutics to patients with high unmet medical need."

"Collaborations with companies such as GSK are an integral part of our strategy to build a new leading biopharm company that commercializes products in the United States," said Jason Rhodes, Executive Vice President and Chief Business Officer. "Since January 2011, we have entered into benchmark alliances with GSK, Eisai and Celgene that together have brought in $140 million in cash, with future committed research funding and expected milestones. Importantly, Epizyme retains significant U.S. rights to our lead DOT1L and EZH2 programs, which are partnered with Celgene and Eisai, respectively, in addition to our pipeline of unpartnered programs."

The GSK alliance leverages Epizyme's unique product platform – including its proprietary biology, biochemistry, medicinal chemical, and intellectual property – to discover and develop HMT therapeutics against the defined set of targets included in the collaboration. Under the terms of the agreement, Epizyme received an upfront payment of $20 million and also receives committed research funding. Epizyme is eligible to receive more than $630 million in total milestone payments if medicines are commercialized for all targets in the collaboration. Additionally, Epizyme is eligible to receive up to double-digit royalties on worldwide net sales of collaboration products. For each collaboration target, Epizyme is primarily responsible for research up to development candidate selection, and GSK will be solely responsible for development and commercialization.

The HMT class of epigenetic enzymes contains 96 members, many of which have strong genetic associations with cancer and other serious diseases. Targeting HMTs with potent and selective small molecule inhibitors (HMTi) offers an innovative therapeutic approach to controlling pathways of disease-causing gene expression and to the creation of personalized therapeutics for patients with genetically defined diseases.

About Epizyme
Epizyme is leading the creation of small molecule histone methyltransferase inhibitors (HMTi), a new class of personalized therapeutics for patients with genetically defined cancers. Genetic alterations in HMTs, a family of epigenetic enzymes, drive multiple human diseases. Our approach represents the future of healthcare by matching better medicines with the right patients.

Epizyme has benchmark alliances with Celgene, GSK and Eisai and receives funding and strategic support from the Multiple Myeloma Research Foundation (MMRF) and the Leukemia & Lymphoma Society (LLS). For more information, visit www.epizyme.com.

SOURCE Epizyme, Inc.